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. Author manuscript; available in PMC: 2020 Oct 21.
Published in final edited form as: ACS Chem Biol. 2013 Aug 15;8(10):2235–2244. doi: 10.1021/cb400495h

Table 4.

Inhibitory Activities (IC50 Values) toward the 3′-End Processing and Strand Transfer Reactions Catalyzed by HIV-1 IN, anti-HIV Activities (EC50 Values, p24 and MTT Assays) and Cytotoxicities (CC50 values, MTT Assay) of the Conjugates of Compound 6S with Oligo-arginine Sequences

peptide IC50 (μM)
3′-end
processing		 IC50 (μM)
strand transfer		 EC50
(μM)
p24
assay		 EC50
(μM)
MTT
assay		 CC50
(μM)
MTT
assay
20 0.45 ± 0.02 0.22 ± 0.02 6.5 3.2 16
21 0.47 ± 0.03 0.21 ± 0.03 3.2 3.1 15
22 0.25 ± 0.01 0.14 ± 0.03 7.4 4.7 13
23 0.18 ± 0.01 0.062 ± 0.005 5.6 27% at 5 μM 12
17 0.17 ± 0.01 0.076 ± 0.009 7.1 28% at 5 μM 6.9
6S 2.6 ± 0.1 0.75 ± 0.08 8.3 6.4 >20
1 2.0 ± 0.2 2.2 ± 0.2 >20 N.T. N.T.
2 0.16 ± 0.05 0.062 ± 0.009 6.4 N.T. N.T.
AZT N.T. N.T. 0.29 0.07 >100